Potentiating 1-(2-hydroxypropyl)-2-styryl-5-nitroimidazole derivatives against antibacterial agents: Design, synthesis and biology analysis

• 20 Novel 2-styryl-5-nitroimidazole derivatives have been synthesized.
• Their biological activities were evaluated against bacterial.
• Most of the compounds showed low toxicity to human macrophage cells.
• Compound 30 showed the most potent and best selective Escherichia coli FabH inhibition.
• Crystal structure of compounds 32, 33 and 34 were determined.

A series of novel 1-(2-hydroxypropyl)-2-styryl-5-nitroimidazole derivatives had been designed, synthesized, isolated and evaluated as potentiators of antibacterial agents. All these synthesized compounds were determined by elemental analysis, 1H NMR, and MS. Their biological activities were also evaluated against two Gram-negative bacterial strains: Escherichia coli and Pseudomonas aeruginosa and two Gram-positive bacterial strains: Bacillus thuringiensis and Bacillus subtilis by MTT method as potential FabH inhibitory. The results showed that compound 30 exhibited the most potent E. coli FabH inhibitory activity with IC50 of 4.6 μM. Molecular modeling simulation studies were performed in order to predict the biological activities of the proposed compounds. All compounds have been tested for toxicity by MTT assay on human macrophage.

A new series of nove1-(2-hydroxypropyl)-2-styryl-5-nitroimidazole derivatives had been designed, synthesized, isolated and evaluated as potentiators of against bacterial agents. Compound 30 exhibited the most potent Escherichia coli FabH inhibitory activity.Figure optionsDownload as PowerPoint slide